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175 Cards in this Set
- Front
- Back
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T/F high Km means high affinity
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false
high Km means low affinity |
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Competitive vs noncompetitive inhibitors
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competitive:
resemble substrate overcome by increase substrate bind active site does not affect Vmax increases Km decreases potency |
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T/F noncompetitive inhibitors decrease potency of the drug
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false - decreases efficacy
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volume of distribution
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amount of drug in body compared to plasma concentration
low (4-8L) means distribute in blood only high (greater than body weight) means distributes too all tissues medium - extracellular space |
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how can Vd of plasma protein bound drugs be alterted?
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liver and kidney disease
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clearnace =
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rate of elimination of drug/plasma drug concentration
= Vd x elimination constant Ke |
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half life equation
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0.7 X Vd/CL
1 half life - 50% eliminated 2 half life - 75% eliminated 3 HL - 87.5 4 HL - 93.75 |
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how many half lives does it take for a drug that is constant infused to reach steady state
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4-5
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loading dose
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target plasma concentration x Vd/bioavailability
bioavailability = F = 1 if its given IV |
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mintenance dose
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target plasma concentration x CL/bioavailability
bioavailability = F = 1 if its given IV |
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zero order elimination
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rate of elimination is constant regardless of concentration in plasma
Phenytoin ethanol aspirin linear elimination graph |
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first order elimination
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elimination rate depends on concentration
hyperbolic elimination graph |
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how do you treat overdose of a weak acidic drug
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bicarbonate
example: phenobarbitol, mehtotrexate, asprine |
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how to treat overdose of weak basic drug
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ammonium chloride
example: amphetamine |
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Phase I metabolism
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done by Cyto P450
reduction, oxudation, hydrolysis drug often still active, but a bit more polar to aid excretion |
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Phase II metabolism
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conjugation reaction
acetylation, glucuronidation, sulfation - yields very polar, inactive metabolite |
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effficacy of drug
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maximal effect of a drug
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potency of drug
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amount of drug needed for a given effect
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competitive antagonist
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shifts dose effect curve to right
decreases potency without effect on efficacy |
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noncompetitive antagonist
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shifts effect dose curve down
decreases efficacy |
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partial agonist
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acts at same site as full agonist - but reduced maximal effect
decreases efficacy potency can increase or decrease |
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physiologic antagonism
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substance that produces the opposite physiologic effect of an agonist - but not at same recetpor
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therapeutic index
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medial lethal dose/median effective dose = LD50/ED50
safer drugs have higher TI |
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nicotinic vs muscarinic ACh receptors
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nicotinic are Na+/K+ ligand gated channels (Nn and Nm subtypes)
muscarinic are G Protein mediated (5 subtypes M1-M5) |
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renal vascular smooth muscle is acted upon with what neurotransmitter at the nerve terminal
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Dopamine
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cardiac/smooth muscle are acted upon by what kind of neurotransmitter at the postganglionic nerve terminal
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Norepinephrine alpha and beta
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where do you see cholinergic nicotinic fibers
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preganglionic fibers
adrenal medulla sketal muscle |
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general effects of alpha1
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increased vascular smooth muscle contraction
increased pupullary dilator muscle contraction (mydriasis) increased intestinal and bladder sphincter contraction |
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general effects of alpha2
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decreased sympathetic outlfow (inhibits NE release)
decreased insulin release |
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general effects of beta1
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increased heart rate, heart contractility
increased renin release increased lipolysis |
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general effects of beta2
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vasodilation, brohcodilation
increased heart rate (2ndary effect) increased contractility (2ndary effect) |
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general effects of M1
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parasympathetic
CNS and enteric nervous system |
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general effects of M2
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parasympathetic
decreased heart rate and contractility of atria |
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general effects of M3
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parasympathetic
increased exocrine gland secretion increased gut parastalsis increased bladder contraction bronchoconstriction increased pupullar sphincter muslce contraction (miosis) ciliary muscle contraction (accomodation) |
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general effects of D1
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dopamine
relaxes renal vascular smooth muscle |
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general effects of D2
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dopamine
modulates transmitter release |
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general effects of H1
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histamine
increased nasal and bronchial mucus production contraction of bronchioles puritis pain |
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general effects of H2
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histamine
increased gastric acid |
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general effects of V1
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vasopressin
increased vascular smooth muscle contraction |
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general effects of V2
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increased H2O perm and reabsorption in collecting tubules of kidney
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subtypes of G protines
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Gq - phospholipase C
Gs - activates adenylyl cyclase Gi - inhibits adenlyl cyclase |
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which receptors are associated with Gq
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alpha1, H1, V1, M1, M3
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which receptors are associated with Gs
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beta1,beta1, D1, H2, V2
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which receptors are assoicated with Gi
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M2, alpha2, D2
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which receptors are associated with Gq
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alpha1, H1, V1, M1, M3
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which receptors are associated with Gs
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beta1,beta1, D1, H2, V2
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which receptors are assoicated with Gi
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M2, alpha2, D2
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which receptors are associated with Gq
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alpha1, H1, V1, M1, M3
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which receptors are associated with Gs
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beta1,beta1, D1, H2, V2
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which receptors are assoicated with Gi
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M2, alpha2, D2
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vesamicol
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blocks acetylcholine presynaptically by inhibiting achetylecholine receptor for secretory vesicle packaging
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hemicholinum
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inhibits choline uptake into presymaptic terminal preventing ACh prudction
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metyrosine
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blocks tyrosine conversion to DOPA in presympatic
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reserpine
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inhibits receptor necessary for dopamine packaging in secretory vesicles
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guanethidine
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inhibits norepinephrine release by replacing neorepinephrine in the secretory vesicle
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amphetamines
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increase NE and dopamine release by revesing VMAT transport allowing NE and dopamine to escape the vesicle and be released through the terminal
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cocaine, TCAs, amphetamines effect
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blocks reuptake of NE leaving it in the synaptic cleft
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bethanechol
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postoperative and neurogenic ileus and urinary retention
cholinomimetic - direct activates Bowel and Bladder smooth muscle |
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carbachol
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cholinomimetic - direct
glaucoma, pupillary contraction, relief of intraocular pressure |
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pilocarpine
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cholinomimetic - direct
stimulator of sweat, tears, saliva acts to conttract ciliary muscle of eye (open angle glaucoma) and pupillary sphincter (closed angle glaucoma) |
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methacholine
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cholinomimetic - direct agonist
challenge test for diagnosis of asthma |
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neostigmine
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Cholinomimietic - indirect - anticholinetesterase
postop and neurogenic ileus, urinary retention, myasthenia gravis, neveral of neuro-mus junction block increases endogenous Ach no effect on CNS cannot penetrate |
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Pyridostigmine
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Cholinomimietic - indirect - anticholinetesterase
myasthenia gravis (long acting) no CNS effect |
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edrophonium
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Cholinomimietic - indirect - anticholinetesterase
diagnosis of myasthenia gravis (short acting) |
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physostigmine
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Cholinomimietic - indirect - anticholinetesterase
glaucoma crosses BBB - CNS effects |
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echothiophate
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Cholinomimietic - indirect - anticholinetesterase
glaucoma |
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what conditions must you watch for with cholinomemetics?
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COPD
asthma PUD |
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parathion
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organophosphate - irreversible inhibit AchE
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cholinesterase inhibitor poisoning
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causes diarrhea, urination, miosis, bronchiospasm, bradycardia, excitation of skeletal muscle and CNS, lacrimation, sweating, salivation
BUMBBELSS treat with atropine + pralidoxime |
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atropine
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muscarinic acetylcholine antagonist
uses - eye - produces mydriasis and cycloplegia decreases airway secretion decreases stomach secretion decreaes gut motility decreases urgency bladder toxcity: increases body temp by decrease sweat, rapid pulse, dry mouth, flushed skin, constipation, cyclopelegia, disorientation cause acute angle-closure glaucoma, urinary retention with prostatic hyperplasia, hyperthermia |
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Benztropine
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muscarinic acetylcholine antagonist
uses - parkinsons |
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scopalaline
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muscarinic acetylcholine antagonist
motion sickness |
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ipratropium
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muscarinic acetylcholine antagonist
asthma, COPD Ipra - "I pray I can breathe soon) |
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oxybutynin
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muscarinic acetylcholine antagonist
reduce urgency in mild cystitis and bladder spasms |
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methscopalamine, propanthelini
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muscarinic acetylcholine antagonist
PUD treatment |
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hexamethonium
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nicotini antagonist
ganglionic blocker used in experimental models to preven vagal reflex response in changes in BP toxicity: orthostatic hypotension, blurred vision, constipation, sexual dysfunction |
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epinephrine
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sympathomemetics - direct
low dose selective for b1 a1 = a2, b1=b2 applications: anaphylaxis, glaucoma, asthma, hypotension |
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norepinephrine
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sympathomemetics - direct
a1,a2>b2 treat: hypotension |
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isoproterenol
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sympathomemetics - direct
b1=b2 treat: AV block |
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dopamine
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sympathomemetics - direct
D1=D2>beta>alpha inotropic, chronoctropic treatL shock (increases renal perfusion), heart failure |
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dobutamine
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sympathomemetics - direct
beta1> beta2, inotropic but not chronotropic treats: heart failure, cardiac stress testing |
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phenylephrine
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sympathomemetics - direct
alpha1>alpha2 pupillary dilaiton, vasoconstriction, nasal decongestion |
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metaproternol, albuterol, salmeterol, terbutaline
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sympathomemetics - direct
selective beta2 agonist (beta2>beta1) metaproternol and albuterol - acute asthma salmeterol - long term astham treatment terbutaline - reduce premature uterine contraction |
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ritodrine
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sympathomemetics - direct
beta2 agonist reduces premature uterine contraction |
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amphetamines
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indirect sympathomemetic
indirect general agonist, releases stored catecholamines treats narcoplepsy, obesity, attention deficit disorder |
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ephedrine
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indirect sympathomemetic
indirect general agonist, releases stored catecholamines treats nasal decongestion, urinary incontinence, hypotension |
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cocaine
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indirect sympathomimetic
indirect general agonist, uptake inhibitor |
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clonidine, alpha-methyldopa
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centrally acting alpha2 agonist
decreases central adrenergic outflow treats: hypertension |
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phenoxybenzamine, phentolamine
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nonselective alpha blocker
treatment of pheochromocytoma before removing tumor phenoxybenzamine - irreversible phentolamine - reversible toxicity: orthostatic hypotension, reflex tachycardia |
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prazosin, terzosin, doxazocin
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alpha1 selective blocker
treat: hypertension, urinary retension inf BPH toxicity: 1st dose orthostatic hypotension, dizziness, headache |
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mirtazapine
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alpha2 selective blocker
treats: depression toxicity: sedation, increased cholesterol, increased appetite |
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beta blockers uses
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-lol drugs
treats: hypertension angina pectoris MI SVT (esp, propranolol, esmolol) CHF Glaucoma (timolol) |
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beta blockers toxicity
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impotence
asthma exacerbation bradycardia, AV block, CHF caution with diabetics (inhibits gluconeogenesis and blunts warning symptoms of hypoglycemia) sedation/sleep (CNS effects) |
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nonselective beta blockers
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beta1 = beta2
propranolol timolol nadolol pindolol |
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beta1 selective blocker
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beta1>beta2
acebutolol (partial agonist) betaxolol emolol atenolol metoprolol A Beam of beta1 blockers good for patients with comorbid pulm disease |
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nonselective alpha and beta antagonists
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alpha1 block
beta1 = beta2 block carvedilol labetalol |
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partial beta agonists
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pindolol
acebutolol |
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N-acetylcysteine
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treatment for acetomenophen toxicity
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treatment for salicylates poisoning
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sodium bicarb
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treatment for amphetamines OD
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ammonium chloride
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treatment for organophosphate poison
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atropine, pralidoxime
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partial beta agonists
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pindolol
acebutolol |
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N-acetylcysteine
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treatment for acetomenophen toxicity
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treatment for salicylates poisoning
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sodium bicarb
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treatment for amphetamines OD
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ammonium chloride
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treatment for organophosphate poison
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atropine, pralidoxime
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treatment for antimuscarinic or anticholinergic OD
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physostigmine
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OD beta blocker treatment
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glucagon
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digitalis OD treatment
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stop dig
normalize K+ lidocaine anti-dig fab fragments Mg2++ |
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iron toxicity treatment
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deferoxamine
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lead toxicity treatment
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CaEDTA, dimercaprol, succimer, penicillamine
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Mercury, gold, arcinic poisoning treatment
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dimercaprol, succimer
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copper, arsenic, gold poisoning treamtent
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penicillamine
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cyanide poisning treatment
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nitrite, hydroxocobalimn, thiosulfate
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methemoglobin treatment
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METHyline blue, vit C
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carbon monoxide poisoning treatment
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100% O2, hyperbaric O2
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methanol, ethylene glycol poisoning treatment
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ethanol, dialysis, fomepizole
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opiod overdose treatment
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naloxone/naltrexone
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benzodiazepines poisoning treamtnet
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flumenizil
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TCA poisoning treatment
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soidum bicarbonate
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heparine overdose treatment
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protamine
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warfarin overdose treatment
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vitamin K, fresh frozen plasma
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tPA/streptokinase overdose treatment
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aminocaproic acid
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theophylline overdose treatment
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beta blocker
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coronary vasospasm associated with
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cocaine, sumatriptan
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atropine like side effects associated with
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TCAs
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cutaneous flushing associated with
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Vanco, adenosine, niacine, Ca++ channel blockers
VANC |
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dialated cardiomyopathy associated with
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doxirubicin, daunorubicin
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torsades de points associated with
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Class III antoarryhtmics - sotalol
class1A antiarryhtmics - quniidine |
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agranulocytosis associated with
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cloazapine
carbamazepine colchisine propylthiouracil methimazole dapsone |
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aplastic anemia associated with
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chloramphenicol, benzine, NSAIDS, propylthiouracil, methimazole
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direct coombs positive hemolytic anemia associated with
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methyldopa
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gray baby sydrome associated with
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chloramphenocol
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hemolysis in G6PD deficient patients associated with
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hemolysis IS PAIN
isoniazid sulfonamides primaquine asprin ibuprofen nitrofurantoin |
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megaloblastic anemia associated with
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having a blast with MPS
phenytoin methotrexate sulfas |
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thrombotic complications associated with
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oral contraceptives
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cough associated with with drugs
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ACE inhibitors
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pulmonary fibrosis associated with with drugs
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BLeomycin
Amiodarone busulfan hard to BLAB when you have pulmonary fibrosis |
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acute cholestatic hepatitis associated with with drugs
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macrolides - erythromycin
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focal-massive hepatic necrosis associated with with drugs
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halothane, valproic acid, acetaminophen, amanita phalloides
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hepatitis associated with with drugs
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isonizid
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pseudomembranous colitis associated with with drugs
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clindamycin, ampicillin
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adrenocortical insuff associated with with drugs
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glucocorticoid withdrawl
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gynecomastia associated with with drugs
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spironolactone
digitalis cimetidine alcohol estrogens Ketoconazole some drugs create awesome knockers |
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hot flashes associated with with drugs
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tamoxifen, clomiphene
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hypothyroidism associated with with drugs
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lithium, amiodarone
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gingival hyperplasia associated with with drugs
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phenytoin
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gout associated with which drugs
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furosamide, thiazides
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osteoporosis associated with with drugs
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heparin, glucocorticoids
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photosensitivity associated with with drugs
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sulfonamides
amiodarone tetracycline (SAT for a photo) |
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Steven Johnson sydrome rash associated with with drugs
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ethosuxamide
lamotirine carbamazepine phenobarb phenytoin sulfa drugs penicillin allopurinol |
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SLE like syndrome associated with with drugs
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hydralizine
isoniazid procainamide phenytoin not HIPP to have lupus |
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tendonitis, tendon ruptures associated with with drugs
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fluroquinolones (kids)
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fanconi syndrome associated with with drugs
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expired tetracycline
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interstitial nephritis associated with with drugs
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methicillin
NSAIDS furosemide |
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hemorrhagic cystitis associated with with drugs
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cyclophosphamide
ifosfamide prevent with mensa administration |
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SLE like syndrome associated with with drugs
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hydralizine
isoniazid procainamide phenytoin not HIPP to have lupus |
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tendonitis, tendon ruptures associated with with drugs
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fluroquinolones (kids)
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fanconi syndrome associated with with drugs
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expired tetracycline
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interstitial nephritis associated with with drugs
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methicillin
NSAIDS furosemide |
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hemorrhagic cystitis associated with with drugs
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cyclophosphamide
ifosfamide prevent with mensa administration |
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cinchonism associated with with drugs
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quinidine, quinine
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diabetes insipitus associated with with drugs
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lithium
demeclocycline |
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parkinson like syndrome associated with with drugs
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halperidol (typical antispychotic)
chlorpromazine reserpine metoclopramide |
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seizures associated with which drugs
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buproprion
imipenem/cilastatin isoniazid |
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tardive dyskinesia associated with which drugs
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antispsychotics
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disulfiram like reaction associated with which drugs
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metronidazole
cephalosporins procarbazine 1st gen sulfonylureas |
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nephrotoxicity with neurotoxicty associated with which drugs
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polymyxins
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nephrotoxicty with ototoxicity associated with which drugs
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aminoglycosides
vancomyclin loop diuretics cisplatin |
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inducers of cyto P450
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Quinidine
Barbituates St. John's Wart Phenytoin Rifampin Griseofulvin Carbamazepine Chronic alchohol |
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inhibitors of cyto P450
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HIV protease inhibitors
Ketoconazole Erythromycin Grapefruit juice Acute alch use sulfonamides Isoniazid Cimetidne |
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mechanism of ethelyene glycol toxicity
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converted to oxalic acid -> acidosis, nephrotoxicity
via alcohol dehydrogenase |
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mechanism of methanol toxicity
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converted to formaldehyde and formic acid -> acidosis, blindness (retinal dmg)
via alcohol dehydrogenase |
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mechanism of acidosis and fatty liver in alcohol toxicity
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alcohol dehydrogenase reaction depletes NAD+ needed for fatty acid oxidayion and conversion of lactic acid to pyruvate ----> lactic acidosis, fatty liver
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sulfa drugs
|
watch for allergies
celecoxib furosemide probenecid thiazide TMP-SMX sulasalzine sulfonylureas acetazolamide sulfonamide antibiotics |
